BE865923A - Excipient a base de cellulose microcristalline pour compositions pharmaceutiques - Google Patents
Excipient a base de cellulose microcristalline pour compositions pharmaceutiquesInfo
- Publication number
- BE865923A BE865923A BE186747A BE186747A BE865923A BE 865923 A BE865923 A BE 865923A BE 186747 A BE186747 A BE 186747A BE 186747 A BE186747 A BE 186747A BE 865923 A BE865923 A BE 865923A
- Authority
- BE
- Belgium
- Prior art keywords
- emi
- excipient
- weight
- powder
- pharmaceutical composition
- Prior art date
Links
- 239000000546 pharmaceutical excipient Substances 0.000 title claims description 58
- 229920000168 Microcrystalline cellulose Polymers 0.000 title claims description 43
- 235000019813 microcrystalline cellulose Nutrition 0.000 title claims description 43
- 239000008108 microcrystalline cellulose Substances 0.000 title claims description 43
- 229940016286 microcrystalline cellulose Drugs 0.000 title claims description 43
- 239000008194 pharmaceutical composition Substances 0.000 title claims description 28
- 239000000843 powder Substances 0.000 claims description 89
- 239000000654 additive Substances 0.000 claims description 8
- 239000004480 active ingredient Substances 0.000 claims description 7
- 238000006116 polymerization reaction Methods 0.000 claims description 7
- 229920000742 Cotton Polymers 0.000 claims description 6
- 239000000126 substance Substances 0.000 claims description 6
- 238000005903 acid hydrolysis reaction Methods 0.000 claims description 3
- 239000000835 fiber Substances 0.000 claims description 3
- 238000010525 oxidative degradation reaction Methods 0.000 claims description 3
- 230000000284 resting effect Effects 0.000 claims 1
- 239000000203 mixture Substances 0.000 description 61
- 239000002075 main ingredient Substances 0.000 description 41
- 239000002775 capsule Substances 0.000 description 36
- 239000008187 granular material Substances 0.000 description 27
- 238000000034 method Methods 0.000 description 24
- 238000007907 direct compression Methods 0.000 description 17
- 239000011230 binding agent Substances 0.000 description 15
- 238000007906 compression Methods 0.000 description 15
- 230000006835 compression Effects 0.000 description 14
- 239000002245 particle Substances 0.000 description 14
- 238000004519 manufacturing process Methods 0.000 description 12
- 238000000576 coating method Methods 0.000 description 11
- 230000008569 process Effects 0.000 description 11
- 239000000047 product Substances 0.000 description 11
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 10
- 239000011248 coating agent Substances 0.000 description 10
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 9
- 239000003795 chemical substances by application Substances 0.000 description 8
- 238000011049 filling Methods 0.000 description 8
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 8
- 239000000243 solution Substances 0.000 description 7
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 6
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 6
- 230000000694 effects Effects 0.000 description 6
- 238000001914 filtration Methods 0.000 description 6
- 239000004615 ingredient Substances 0.000 description 6
- 239000008101 lactose Substances 0.000 description 6
- 238000012360 testing method Methods 0.000 description 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 5
- 239000002253 acid Substances 0.000 description 5
- 229960005070 ascorbic acid Drugs 0.000 description 5
- 235000010323 ascorbic acid Nutrition 0.000 description 5
- 239000011668 ascorbic acid Substances 0.000 description 5
- 230000015572 biosynthetic process Effects 0.000 description 5
- 239000011362 coarse particle Substances 0.000 description 5
- 239000006185 dispersion Substances 0.000 description 5
- 238000005469 granulation Methods 0.000 description 5
- 230000003179 granulation Effects 0.000 description 5
- 238000012856 packing Methods 0.000 description 5
- 230000009467 reduction Effects 0.000 description 5
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 4
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 4
- 239000000428 dust Substances 0.000 description 4
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 4
- 235000019359 magnesium stearate Nutrition 0.000 description 4
- 238000002156 mixing Methods 0.000 description 4
- 238000005550 wet granulation Methods 0.000 description 4
- 239000011575 calcium Substances 0.000 description 3
- 239000001506 calcium phosphate Substances 0.000 description 3
- 229910000389 calcium phosphate Inorganic materials 0.000 description 3
- 235000011010 calcium phosphates Nutrition 0.000 description 3
- 239000010419 fine particle Substances 0.000 description 3
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 3
- 230000001771 impaired effect Effects 0.000 description 3
- 239000003456 ion exchange resin Substances 0.000 description 3
- 229920003303 ion-exchange polymer Polymers 0.000 description 3
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 3
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 3
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 3
- 238000000926 separation method Methods 0.000 description 3
- 239000007921 spray Substances 0.000 description 3
- 239000003826 tablet Substances 0.000 description 3
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 3
- NWUYHJFMYQTDRP-UHFFFAOYSA-N 1,2-bis(ethenyl)benzene;1-ethenyl-2-ethylbenzene;styrene Chemical compound C=CC1=CC=CC=C1.CCC1=CC=CC=C1C=C.C=CC1=CC=CC=C1C=C NWUYHJFMYQTDRP-UHFFFAOYSA-N 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- 229920000297 Rayon Polymers 0.000 description 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 2
- 229920002472 Starch Polymers 0.000 description 2
- 238000010521 absorption reaction Methods 0.000 description 2
- 230000000996 additive effect Effects 0.000 description 2
- 239000007864 aqueous solution Substances 0.000 description 2
- 230000008901 benefit Effects 0.000 description 2
- 230000000903 blocking effect Effects 0.000 description 2
- 238000000748 compression moulding Methods 0.000 description 2
- 238000005336 cracking Methods 0.000 description 2
- 238000000151 deposition Methods 0.000 description 2
- 238000004090 dissolution Methods 0.000 description 2
- 238000009826 distribution Methods 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 239000000706 filtrate Substances 0.000 description 2
- 244000144992 flock Species 0.000 description 2
- 230000006872 improvement Effects 0.000 description 2
- 239000008011 inorganic excipient Substances 0.000 description 2
- 239000002655 kraft paper Substances 0.000 description 2
- 229940126601 medicinal product Drugs 0.000 description 2
- 238000000465 moulding Methods 0.000 description 2
- 238000004806 packaging method and process Methods 0.000 description 2
- 239000000825 pharmaceutical preparation Substances 0.000 description 2
- CPJSUEIXXCENMM-UHFFFAOYSA-N phenacetin Chemical compound CCOC1=CC=C(NC(C)=O)C=C1 CPJSUEIXXCENMM-UHFFFAOYSA-N 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- 239000002964 rayon Substances 0.000 description 2
- 238000007873 sieving Methods 0.000 description 2
- 239000002002 slurry Substances 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- 235000019698 starch Nutrition 0.000 description 2
- VZSRBBMJRBPUNF-UHFFFAOYSA-N 2-(2,3-dihydro-1H-inden-2-ylamino)-N-[3-oxo-3-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)propyl]pyrimidine-5-carboxamide Chemical compound C1C(CC2=CC=CC=C12)NC1=NC=C(C=N1)C(=O)NCCC(N1CC2=C(CC1)NN=N2)=O VZSRBBMJRBPUNF-UHFFFAOYSA-N 0.000 description 1
- WZFUQSJFWNHZHM-UHFFFAOYSA-N 2-[4-[2-(2,3-dihydro-1H-inden-2-ylamino)pyrimidin-5-yl]piperazin-1-yl]-1-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)ethanone Chemical compound C1C(CC2=CC=CC=C12)NC1=NC=C(C=N1)N1CCN(CC1)CC(=O)N1CC2=C(CC1)NN=N2 WZFUQSJFWNHZHM-UHFFFAOYSA-N 0.000 description 1
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 1
- 229920002261 Corn starch Polymers 0.000 description 1
- 108010010803 Gelatin Proteins 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 1
- 238000005299 abrasion Methods 0.000 description 1
- 238000002835 absorbance Methods 0.000 description 1
- 230000002378 acidificating effect Effects 0.000 description 1
- 238000005054 agglomeration Methods 0.000 description 1
- 230000002776 aggregation Effects 0.000 description 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
- 229910052791 calcium Inorganic materials 0.000 description 1
- 235000010980 cellulose Nutrition 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 239000007795 chemical reaction product Substances 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 239000008120 corn starch Substances 0.000 description 1
- 238000010908 decantation Methods 0.000 description 1
- 230000007547 defect Effects 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- 239000002612 dispersion medium Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 238000007905 drug manufacturing Methods 0.000 description 1
- 229940126534 drug product Drugs 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 238000001125 extrusion Methods 0.000 description 1
- 239000012065 filter cake Substances 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 235000001727 glucose Nutrition 0.000 description 1
- 238000000227 grinding Methods 0.000 description 1
- 230000007062 hydrolysis Effects 0.000 description 1
- 238000006460 hydrolysis reaction Methods 0.000 description 1
- 229910052500 inorganic mineral Inorganic materials 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 239000011777 magnesium Substances 0.000 description 1
- 229910052749 magnesium Inorganic materials 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 239000011707 mineral Substances 0.000 description 1
- 239000004482 other powder Substances 0.000 description 1
- 229960003893 phenacetin Drugs 0.000 description 1
- 229920003023 plastic Polymers 0.000 description 1
- 239000004033 plastic Substances 0.000 description 1
- 239000011148 porous material Substances 0.000 description 1
- 238000012545 processing Methods 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 238000010298 pulverizing process Methods 0.000 description 1
- 238000004080 punching Methods 0.000 description 1
- 238000011084 recovery Methods 0.000 description 1
- 238000005204 segregation Methods 0.000 description 1
- 238000004904 shortening Methods 0.000 description 1
- 238000005029 sieve analysis Methods 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 238000003828 vacuum filtration Methods 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Inorganic Chemistry (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP4154577A JPS53127553A (en) | 1977-04-13 | 1977-04-13 | Vehicle |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BE865923A true BE865923A (fr) | 1978-10-12 |
Family
ID=12611382
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BE186747A BE865923A (fr) | 1977-04-13 | 1978-04-12 | Excipient a base de cellulose microcristalline pour compositions pharmaceutiques |
Country Status (2)
| Country | Link |
|---|---|
| JP (1) | JPS53127553A (cs) |
| BE (1) | BE865923A (cs) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS6048934A (ja) * | 1983-08-29 | 1985-03-16 | Daicel Chem Ind Ltd | 錠剤用粉粒体組成物 |
| JPS62240302A (ja) * | 1986-04-10 | 1987-10-21 | Asahi Chem Ind Co Ltd | 超低分子量セルロ−スの調製法 |
| JPH035947U (cs) * | 1989-05-31 | 1991-01-21 | ||
| WO2004073729A1 (ja) | 2003-02-21 | 2004-09-02 | Translational Research Ltd. | 薬物の経鼻投与用組成物 |
| USRE45404E1 (en) | 2003-03-27 | 2015-03-03 | Shin Nippon Biomedical Laboratories, Ltd. | Powder medicine applicator for nasal cavity |
| BRPI0507139A (pt) | 2004-01-30 | 2007-06-19 | Asahi Kasei Chemicals Corp | agregado de celulose porosa, processo para produzir o mesmo, e composição de produto moldado |
| JP2005232260A (ja) * | 2004-02-18 | 2005-09-02 | Asahi Kasei Chemicals Corp | セルロース無機化合物多孔質複合粒子 |
| JP2005255617A (ja) * | 2004-03-11 | 2005-09-22 | Asahi Kasei Chemicals Corp | 微粒子状活性成分および多孔質セルロース凝集体含有固形製剤組成物 |
| JP2005255619A (ja) * | 2004-03-11 | 2005-09-22 | Asahi Kasei Chemicals Corp | 昇華性活性成分および多孔質セルロース粒子含有固形製剤組成物 |
| JP2005255616A (ja) * | 2004-03-11 | 2005-09-22 | Asahi Kasei Chemicals Corp | 液状、半固形状活性成分および多孔質セルロース凝集体粒子含有固形製剤組成物 |
| JP2005255618A (ja) * | 2004-03-11 | 2005-09-22 | Asahi Kasei Chemicals Corp | 水難溶性活性成分および多孔質セルロース粒子含有固形製剤組成物。 |
| US8673360B2 (en) | 2004-08-10 | 2014-03-18 | Shin Nippon Biomedical Laboratories, Ltd. | Compositions that enable rapid-acting and highly absorptive intranasal administration |
| US8153157B2 (en) | 2005-04-22 | 2012-04-10 | Asahi Kasei Chemicals Corporation | Porous cellulose aggregate and molding composition thereof |
| US8106100B2 (en) | 2005-12-06 | 2012-01-31 | Asahi Kasei Chemicals Corporation | Process for producing tablet by high-speed direct compression |
| CN101668544B (zh) | 2006-12-26 | 2013-04-24 | 株式会社新日本科学 | 经鼻投用制剂 |
| US8367115B2 (en) | 2007-08-27 | 2013-02-05 | Asahi Kasei Chemicals Corporation | Process for production of crystalline cellulose and tablets containing granules |
| JP5439366B2 (ja) | 2008-05-21 | 2014-03-12 | 旭化成ケミカルズ株式会社 | 偏析防止効果に優れるセルロース粉末及びその組成物 |
| US9101539B2 (en) | 2009-05-15 | 2015-08-11 | Shin Nippon Biomedical Laboratories, Ltd. | Intranasal pharmaceutical compositions with improved pharmacokinetics |
| GB2472327B (en) | 2009-07-31 | 2013-03-13 | Shin Nippon Biomedical Lab Ltd | Intranasal granisetron and nasal applicator |
| JP5731708B2 (ja) * | 2011-04-06 | 2015-06-10 | ダウ グローバル テクノロジーズ エルエルシー | 新規多糖類誘導体及び剤形 |
| US10662258B2 (en) | 2012-05-31 | 2020-05-26 | Asahi Kasei Chemicals Corporation | Cellulose powder |
| WO2013180248A1 (ja) * | 2012-05-31 | 2013-12-05 | 旭化成ケミカルズ株式会社 | セルロース粉末 |
| US11744967B2 (en) | 2017-09-26 | 2023-09-05 | Shin Nippon Biomedical Laboratories, Ltd. | Intranasal delivery devices |
-
1977
- 1977-04-13 JP JP4154577A patent/JPS53127553A/ja active Granted
-
1978
- 1978-04-12 BE BE186747A patent/BE865923A/fr not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| JPS5638128B2 (cs) | 1981-09-04 |
| JPS53127553A (en) | 1978-11-07 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| RE20 | Patent expired |
Owner name: FMC CORP. Effective date: 19980412 |